Cryo-EM reveals an unprecedented binding site for NaV1. 7 inhibitors enabling rational design of potent hybrid inhibitors
M Kschonsak, CC Jao, CP Arthur, AL Rohou… - Elife, 2023 - elifesciences.org
The voltage-gated sodium (NaV) channel NaV1. 7 has been identified as a potential novel
analgesic target due to its involvement in human pain syndromes. However, clinically …
analgesic target due to its involvement in human pain syndromes. However, clinically …
Molecular basis of opioid action: From structures to new leads
A Manglik - Biological psychiatry, 2020 - Elsevier
Since the isolation of morphine from the opium poppy over 200 years ago, the molecular
basis of opioid action has remained the subject of intense inquiry. The identification of …
basis of opioid action has remained the subject of intense inquiry. The identification of …
[HTML][HTML] The impact of the secondary binding pocket on the pharmacology of class A GPCRs
G-protein coupled receptors (GPCRs) are considered important therapeutic targets due to
their pathophysiological significance and pharmacological relevance. Class A receptors …
their pathophysiological significance and pharmacological relevance. Class A receptors …
[HTML][HTML] Recent advances in structure, function, and pharmacology of class A lipid GPCRs: opportunities and challenges for drug discovery
Great progress has been made over the past decade in understanding the structural,
functional, and pharmacological diversity of lipid GPCRs. From the first determination of the …
functional, and pharmacological diversity of lipid GPCRs. From the first determination of the …
[PDF][PDF] Cryo-EM structure of the β3-adrenergic receptor reveals the molecular basis of subtype selectivity
C Nagiri, K Kobayashi, A Tomita, M Kato, K Kobayashi… - Molecular Cell, 2021 - cell.com
The β 3-adrenergic receptor (β 3 AR) is predominantly expressed in adipose tissue and
urinary bladder and has emerged as an attractive drug target for the treatment of type 2 …
urinary bladder and has emerged as an attractive drug target for the treatment of type 2 …
Different conformational responses of the β2-adrenergic receptor-Gs complex upon binding of the partial agonist salbutamol or the full agonist isoprenaline
G protein-coupled receptors (GPCRs) are responsible for most cytoplasmic signaling in
response to extracellular ligands with different efficacy profiles. Various spectroscopic …
response to extracellular ligands with different efficacy profiles. Various spectroscopic …
GPCR allosteric modulator discovery
G protein-coupled receptors (GPCRs) influence virtually every aspect of human physiology;
about one-third of all marketed drugs target members of this family. GPCR allosteric ligands …
about one-third of all marketed drugs target members of this family. GPCR allosteric ligands …
[HTML][HTML] Pharmacological targeting of G protein-coupled receptor heteromers
E Moreno, N Casajuana-Martin, M Coyle… - Pharmacological …, 2022 - Elsevier
A main rationale for the role of G protein-coupled receptor (GPCR) heteromers as targets for
drug development is the putative ability of selective ligands for specific GPCRs to change …
drug development is the putative ability of selective ligands for specific GPCRs to change …
Strategies for the discovery of biased GPCR ligands
M Bermudez, TN Nguyen, C Omieczynski… - Drug Discovery …, 2019 - Elsevier
Highlights•Biased GPCR modulators provide various therapeutic benefits.•The number of
newly identified biased ligands is constantly increasing.•Understanding underlying receptor …
newly identified biased ligands is constantly increasing.•Understanding underlying receptor …
Discovery of dual-target ligands binding to beta2-adrenoceptor and cysteinyl-leukotriene receptor for the potential treatment of asthma from natural products derived …
Q Liang, H Zuo, T Yang, J Yin, X Huang, J Wang… - European Journal of …, 2022 - Elsevier
The design, synthesis, and discovery of dual-target compounds are considered as a
promising strategy to develop new drugs with improved safety and efficacy compared with …
promising strategy to develop new drugs with improved safety and efficacy compared with …